Aromatase inhibitors are class of drugs that inhibit aromatase, a rate limiting enzyme in the biosynthesis
of estrogens from their corresponding androgens. Estrogens play a vital role in the development and
growth of breast tumors especially in postmenopausal women apart from their important functions in cell
homeostasis. The reduction of estrogen physiological concentration through aromatase inhibition is
one of the most important therapeutic strategies against this cancer type. The third-generation aromatase
inhibitors are now used as first-line therapy in the treatment of early and metastatic breast cancer in
postmenopausal women. However the quest for new class of drugs still stays indispensable to evade the danger
of conceivable rising resistances to existing drugs, toxicity and unwanted side effects due to chronic treatment.
The current review deals with recent advances in understanding of aromatase, its mechanism and
research in the development of various novel chemotypes as aromatase inhibitors. The new challenges
and the fast changing trends in bringing rational approach in aromatase inhibitors to a different level
like research in dual/multiple target enzyme inhibition strategies, radiolabeling of aromatase inhibitors
as theranostic agents; the development of new computational models for complete understanding of
aromatase enzyme and its substrate/ligand interactions will bring in holistic approach to comprehensive
inhibition of aromatase and other relevant enzymes for effective treatment and monitoring of
postmenopausal breast cancer.
Keywords: Aromatase inhibitors, estrogen, breast cancer, dual inhibitors, molecular modeling, radiolabeling.
Rights & PermissionsPrintExport